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This systematic review (2021–2025) analyzes thiazoles and 4-thiazolidinones/thiazolidinediones as widely used scaffolds in anticancer drug design. It compares favored mechanisms for each scaffold, highlights under-studied targets without FDA-approved drugs, and notes gaps in ADMET, safety testing, and mechanistic linkage between proteins and anticancer effects.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":40,"@type":76,"position":81},"https://docshare.wps.com/document/research-report/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/a-review-of-recent-advances-in-the-anticancer-mechanisms-of-activity-of-novel-thiazoles-and-4-thiazolidinones-a-review/354159/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/a-review-of-recent-advances-in-the-anticancer-mechanisms-of-activity-of-novel-thiazoles-and-4-thiazolidinones-a-review/354159.png","ImageObject",300,407,{"name":92,"@type":93},"Nguyễn Văn Học","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-09-24","2026-09-22",true,{"@type":102,"interactionType":103,"userInteractionCount":8},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"What motivates the review of thiazole-based anticancer scaffolds?","Question",{"text":112,"@type":113},"Cancer incidence is projected to rise sharply by 2050, and resistance to current chemotherapeutics remains a major cause of failure. The review frames thiazoles and 4-thiazolidinones/thiazolidinediones as important scaffold candidates for new anticancer compounds.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"Which anticancer mechanisms are emphasized for thiazoles versus 4-thiazolidinones/thiazolidinediones?",{"text":117,"@type":113},"For thiazoles, the review highlights inhibition of serine/threonine protein kinases such as CDK-2 and BRAFV600E. 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Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.  \n1 Department of Synthesis and Technology of Drugs, Faculty of Pharmacy, Medical University of Bialystok, Jana Kili ´nskiego 1, 15-089 Bialystok, Poland; [krzysztof.bielawski@umb.edu.pl](krzysztof.bielawski@umb.edu.pl)  \n2 Department of Biotechnology, Faculty of Pharmacy, Medical University of Bialystok, Jana Kili ´nskiego 1,  \n15-089 Bialystok, Poland; [magdalena.podolak@sd.umb.edu.pl](magdalena.podolak@sd.umb.edu.pl) (M.P.); [anna.bielawska@umb.edu.pl](anna.bielawska@umb.edu.pl) (A.B.)  \n3 Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv, Ukraine  \n4 Molecular Design Center, Danylo Halytsky Lviv National Medical University, Pekarska 69,  \n79010 Lviv, Ukraine  \n5 Department of Biotechnology and Cell Biology, University of Information Technology and Management in Rzeszow, St. Sucharskiego 2, 35-225 Rzeszow, Poland  \n* Correspondence: [rostyslav.dudchak@sd.umb.edu.pl](rostyslav.dudchak@sd.umb.edu.pl) (R.D.); [roman.lesyk@gmail.com](roman.lesyk@gmail.com) (R.L.)  \nAbstract  \nWith global cancer cases projected to reach 35 million by 2050 and drug resistance to existing chemotherapeutic drugs remaining a significant threat in cancer therapy, accounting for up to 90% of chemotherapy failures, the search for novel anticancer compounds continues tobe increasingly important. This systematic review (2021–2025) examined the role of thiazolesand 4-thiazolidinones/thiazolidinediones as popular scaffolds in existing anticancer drug design. While researchers continue to focus on well-established molecular targets, such as EGFR, VEGFR-2, and tubulin, there is a notable difference regarding other preferred choices for thiazoles and 4-thiazolidinones/thiazolidinediones. Among analyzed mechanisms of anticancer activity notably favored for thiazoles was the inhibition of serine/threonine protein kinases (CDK-2, BRAFV600E), while for 4-thiazolidinones/thiazolidinediones more studied were ROS generation and PPARγ activation. Furthermore, less-researched mechanisms of anticancer activity with no FDA-approved drugs such as PTP1B, SIRT2, PKM2, eIF4E, CA XI and XII inhibition for thiazole derivatives and pan-PIM kinase and BAG3 protein inhibition for 4-thiazolidinones/thiazolidinediones were evaluated as well. Notable was the popularity of the multi-targeting approach for modern drug design, with~30% reporting two or more targets for their compounds. Despite these advancements, the review identified critical gaps in ADMET evaluations, safety analyzing against normal human cells and the lack of mechanistic studies connecting the targeted protein and the compounds anticancer effects.  \nKeywords: 4-thiazolidinone; thiazolidinedione; thiazole; anticancer activity  \n1. Introduction  \nThe thiazole (TZ) moiety is an often-utilized scaffold for the synthesis of novel organic structures with various activities due to its distinctive physicochemical properties. It is a five-membered aromatic ring with every atom being in sp2 hybridization, offering a stable, rigid and planar 6-π system with potential substitutions at C2, C4 and C5  \npositions. Substances with a thiazole structure have been actively utilized in medicinal practice and can be divided into the following groups: antibacterial, antiviral, anticancer, anticoagulant, antifungal, and anti-inflammatory. Antibacterial dru","cbCaiv5XyYXj5Amq","https://ap.wps.com/l/cbCaiv5XyYXj5Amq","pdf",3810453,57,"English","# Abstract\n# Keywords\n# 1. Introduction","[{\"question\":\"What motivates the review of thiazole-based anticancer scaffolds?\",\"answer\":\"Cancer incidence is projected to rise sharply by 2050, and resistance to current chemotherapeutics remains a major cause of failure. The review frames thiazoles and 4-thiazolidinones/thiazolidinediones as important scaffold candidates for new anticancer compounds.\"},{\"question\":\"Which anticancer mechanisms are emphasized for thiazoles versus 4-thiazolidinones/thiazolidinediones?\",\"answer\":\"For thiazoles, the review highlights inhibition of serine/threonine protein kinases such as CDK-2 and BRAFV600E. For 4-thiazolidinones/thiazolidinediones, ROS generation and PPARγ activation are more frequently studied.\"},{\"question\":\"What gaps does the review identify despite recent advances?\",\"answer\":\"Key gaps include insufficient ADMET evaluations, limited safety analysis against normal human cells, and a lack of mechanistic studies that connect targeted proteins to observed anticancer effects.\"}]","A Review of Recent Advances in the Anticancer Mechanisms of Activity of Novel Thiazoles and 4-Thiazolidinones - A Review | PDF",1790109291,144]